Article
Pharmacological characterization of tegaserod at the wild type and 124Cys variant of the human 5-HT1B receptor.
Pharmacogenetics and genomics - 1 Jul 2011
Haenisch Britta, Bönisch Heinz
Abstract excerpt
Sumatriptan, an antimigraine drug, causes contraction of human coronary arteries through activation of 5-HT1B receptors which couple to Gi/Go inducing inhibition of adenylate cyclase. At a rare, naturally occurring human receptor variant (124Cys-h5-HT1B), sumatriptan has previously been shown to act as a more potent agonist than at wild-type receptor. Tegaserod, a 5-HT4-receptor agonist, developed for the...
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